Title:Recent Advances in Structure and Function Studies on Human Bitter Taste Receptors
Volume: 13
Issue: 6
Author(s): Sai Prasad Pydi, Jasbir Upadhyaya, Nisha Singh, Rajinder Pal Bhullar and Prashen Chelikani
Affiliation:
Keywords:
G-protein coupled receptors (GPCRs), bitter taste receptors (T2Rs), structure-function analysis, T2R heterologous
expression, T2R ligand binding, T2R receptor activation mechanism(s), bitter blockers, receptor-expressing cells, Extra-Oral Tissues, GPCRs
Abstract: Humans are capable of sensing five basic tastes and of these, bitter taste sensation alone, is mediated by a large
group of 25 cell surface proteins known as, bitter taste receptors (T2Rs). T2Rs belong to the G-protein coupled receptor
(GPCR) superfamily. However, they share little homology with the large subfamily of Class A GPCRs. Very little progress
has been made in understanding the dynamics of T2R activation, and in discovery of molecules that can block (bitter
blockers) T2R activation. Only recently few structure-function studies focused on elucidating the ligand binding mechanisms
of T2Rs have been published. Here we will discuss the roles of conserved amino acids in T2R structure-function,
possible mechanisms of activation of T2Rs, and compare and contrast with the recent crystal structures of the Class A
GPCRs.
